Composition and application of composition to anti-inflammatory drugs

A composition and drug technology, applied in the direction of anti-inflammatory agents, drug combinations, medical preparations containing active ingredients, etc., can solve the problems of low safety and high toxicity

Inactive Publication Date: 2016-02-03
NANJING FUHAIAOSAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compo

Method used

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  • Composition and application of composition to anti-inflammatory drugs
  • Composition and application of composition to anti-inflammatory drugs
  • Composition and application of composition to anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] The preparation of embodiment 1 compound SalviskinoneA

[0015] The preparation method of the compound Salviskinone A (I) refers to the method published by Ayumi Ohsaki et al. (Ayumi Ohsaki et al., 2011. Salviskinone A, aditerpenewithanewskeleton from Salviaprzewalskii. Tetrahedron Letters 52 (2011) 1375-1377).

[0016]

Embodiment 2

[0017] The synthesis of the O-bromoethyl derivative (II) of embodiment 2SalviskinoneA

[0018] Compound I (312 mg, 1.00 mmol) was dissolved in 15 mL of benzene, and tetrabutylammonium bromide (TBAB) (0.08 g), 1,2-dibromoethane (3.760 g, 20.00 mmol) and 6 mL of 50% sodium hydroxide solution. The mixture was stirred at 35 °C for 12 h. After 12 hours, the reaction solution was poured into ice water, extracted twice with dichloromethane immediately, and the organic phase solutions were combined. Then the organic phase solution was washed with water and saturated brine four times successively, then dried with anhydrous sodium sulfate, and finally concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:1.5, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain a brown powder of Compound II (327mg, 78%)...

Embodiment 3

[0023] The synthesis of the O-(imidazolyl) ethyl derivative (III) of embodiment 3SalviskinoneA

[0024] Compound II (209 mg, 0.5 mmol) was dissolved in 30 mL of acetonitrile, anhydrous potassium carbonate (690 mg, 5.0 mmol), potassium iodide (252 mg, 1.5 mmol) and imidazole (870 mg, 10 mmol) were added thereto, and the mixture was heated to reflux for 4 h. After the reaction, the reaction solution was poured into 45 mL of ice water, extracted three times with an equal amount of dichloromethane, and the organic phases were combined. The combined organic phases were successively washed with water and saturated brine, dried over anhydrous sodium sulfate, and concentrated under reduced pressure to remove the solvent to obtain a crude product. The crude product was purified by silica gel column chromatography (mobile phase: petroleum ether / acetone=100:0.2, v / v), the brown concentrated elution band was collected and the solvent was evaporated to obtain compound III as a light brown ...

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PUM

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Abstract

The invention relates to the field of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method of the composition and an application of the composition to preparation of anti-inflammatory drugs. According to the composition and the preparation method of the composition, pharmacology experiments show that the composition achieves the anti-inflammatory effect, and has the value for developing the anti-inflammatory drugs.

Description

technical field [0001] The invention relates to the fields of organic synthesis and medicinal chemistry, in particular to a composition, a preparation method and an application thereof. Background technique [0002] Inflammation occurs locally but can also affect the whole body. Local clinical features are redness, heat, swelling, pain and dysfunction. Redness and heat are due to the expansion of local blood vessels and the acceleration of blood flow due to inflammation. Swelling is caused by local inflammatory hyperemia and exudation of blood flow components. The development of drugs with anti-inflammatory effects is of great significance for the verification of relief and pain relief. [0003] The existing drugs for the treatment of inflammation have the problems of high toxicity and low safety. It is of great value to find compounds or lead compounds from natural products and carry out structural modification to obtain their derivatives, so as to obtain potential drugs...

Claims

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Application Information

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IPC IPC(8): A61K31/4192A61P29/00C07D233/60C07D249/04A61K31/4164
Inventor 王卓婷
Owner NANJING FUHAIAOSAI PHARMA CO LTD
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